1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    Apoptosis
  2. Casein Kinase
    CDK
    Apoptosis
  3. Casein Kinase inhibitor A51

Casein Kinase inhibitor A51 

Cat. No.: HY-123954
Handling Instructions

Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities.

For research use only. We do not sell to patients.

Casein Kinase inhibitor A51 Chemical Structure

Casein Kinase inhibitor A51 Chemical Structure

CAS No. : 2079068-74-7

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10 mM * 1 mL in DMSO USD 440 Ask For Quote & Lead Time
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10 mg USD 680 Ask For Quote & Lead Time
25 mg USD 1350 Ask For Quote & Lead Time
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Description

Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities[1].

IC50 & Target[1]

CKIα

 

CDK7

1.3 nM (Kd)

CDK9

4 nM (Kd)

In Vitro

Similar to CKIα depletion, Casein Kinase inhibitor A51 (0.05-3.2 μM; 18 hours) treatment of RKO cells abolished most of the Ser45 phosphorylation signal and the consecutive GSK3 phosphorylation cascade resulting in stabilization of β-catenin[1].
Casein Kinase inhibitor A51 is highly effective in inducing leukemia cell apoptosis at 160 nM or lower, mostly in correlation to their capacity to stabilize p53[1].
Casein Kinase inhibitor A51 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A51 induces a marked reduction in mRNA expression of MYC and MDM2, yet upregulates the expression of the Wnt targets AXIN2 and CCND1 (Cyclin D1)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 0.08 μM, 0.6 μM, 2 μM
Incubation Time: 6.5 hours
Result: Abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1.
In Vivo

Oral treatment is initiated at 8 days (Casein Kinase inhibitor A51; 5 mg/kg/day) after leukemia cell inoculation, at which the percentage of leukemia cells in the BM is more than 1.5% of all cells. all A51-treated mice have normal organ morphology and histology and normal blood counts[1].
Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A51 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.5-2 hr, Cmax of 1060 ng/mL, T1/2 of 2.5 hr, and area under the curve (AUC) values of 3680 (ng*hr/mL)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

360.88

Formula

C₁₈H₂₅ClN₆

CAS No.
Shipping

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Casein Kinase inhibitor A51
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HY-123954
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